Eglumegad

Eglumegad
(IUPAC) ime
	(1S,2S,5R,6S)-2-aminobiciklo[3.1.0]heksan-2,6-dikarboksilna kiselina
Klinički podaci
Identifikatori
CAS broj	176199-48-7
ATC kod	nije dodeljen
PubChem	213056
UNII	ONU5A67T2S
Hemijski podaci
Formula	C8H11NO4
Mol. masa	185,18 g/mol
InChI
	InChI=1S/C8H11NO4/c9-8(7(12)13)2-1-3-4(5(3)8)6(10)11/h3-5H,1-2,9H2,(H,10,11)(H,12,13)/t3-,4-,5-,8-/m0/s1 ; Key: VTAARTQTOOYTES-RGDLXGNYSA-N
Farmakoinformacioni podaci
Trudnoća	?
Pravni status

Eglumegad (LY354740) je lek koji se istražuje za potencijalnu primenu u treatmanu anksioznosti^[3] i zavisnosti.^[4] On je jedinjenje izvedeno iz glutamata. Njegov način dejstva sugeriše mogući novi mehanizam.^[5]

Mehanizam akcije

Eglumegad deluje kao agonist koji je selektivan za grupu II metabotropnih glutamatnih receptora (mGluR₂_/₃).^[6]^[7] Nalazi o direktnoj interakciji sa dopaminskim D2 receptorima su inkonzistentni.^[8]^[9]

Reference

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Pilc A. LY-354740 (Eli Lilly). IDrugs. 2003 Jan;6(1):66-71.
↑ Kłodzińska A, Chojnacka-Wójcik E, Pałucha A, Brański P, Popik P, Pilc A. Potential anti-anxiety, anti-addictive effects of LY 354740, a selective group II glutamate metabotropic receptors agonist in animal models. Neuropharmacology. 1999 Dec;38(12):1831-9.
↑ Monn JA, Valli MJ, Massey SM, Wright RA, Salhoff CR, Johnson BG, Howe T, Alt CA, Rhodes GA, Robey RL, Griffey KR, Tizzano JP, Kallman MJ, Helton DR, Schoepp DD. Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic properties. Journal of Medicinal Chemistry. 1997 Feb 14;40(4):528-37.
↑ Schoepp DD, Johnson BG, Wright RA, Salhoff CR, Mayne NG, Wu S, Cockerman SL, Burnett JP, Belegaje R, Bleakman D, Monn JA. LY354740 is a potent and highly selective group II metabotropic glutamate receptor agonist in cells expressing human glutamate receptors. Neuropharmacology. 1997 Jan;36(1):1-11.
↑ Bond A, Monn JA, Lodge D. A novel orally active group 2 metabotropic glutamate receptor agonist: LY354740. Neuroreport. 1997 Apr 14;8(6):1463-6.
↑ Seeman P, Caruso C, Lasaga M (February 2008). „Dopamine partial agonist actions of the glutamate receptor agonists LY 354,740 and LY 379,268”. Synapse 62 (2): 154–8. DOI:10.1002/syn.20482. PMID 18000815.
↑ Fell MJ, Perry KW, Falcone JF, et al. (December 2009). „In vitro and in vivo evidence for a lack of interaction with dopamine D2 receptors by the metabotropic glutamate 2/3 receptor agonists 1S,2S,5R,6S-2-aminobicyclo[3.1.0hexane-2,6-bicaroxylate monohydrate (LY354740) and (-)-2-oxa-4-aminobicyclo[3.1.0] Hexane-4,6-dicarboxylic acid (LY379268)”]. J. Pharmacol. Exp. Ther. 331 (3): 1126–36. DOI:10.1124/jpet.109.160598. PMID 19755662.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Pilc A. LY-354740 (Eli Lilly). IDrugs. 2003 Jan;6(1):66-71.

[4] Kłodzińska A, Chojnacka-Wójcik E, Pałucha A, Brański P, Popik P, Pilc A. Potential anti-anxiety, anti-addictive effects of LY 354740, a selective group II glutamate metabotropic receptors agonist in animal models. Neuropharmacology. 1999 Dec;38(12):1831-9.

[5] Monn JA, Valli MJ, Massey SM, Wright RA, Salhoff CR, Johnson BG, Howe T, Alt CA, Rhodes GA, Robey RL, Griffey KR, Tizzano JP, Kallman MJ, Helton DR, Schoepp DD. Design, synthesis, and pharmacological characterization of (+)-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylic acid (LY354740): a potent, selective, and orally active group 2 metabotropic glutamate receptor agonist possessing anticonvulsant and anxiolytic properties. Journal of Medicinal Chemistry. 1997 Feb 14;40(4):528-37.

[6] Schoepp DD, Johnson BG, Wright RA, Salhoff CR, Mayne NG, Wu S, Cockerman SL, Burnett JP, Belegaje R, Bleakman D, Monn JA. LY354740 is a potent and highly selective group II metabotropic glutamate receptor agonist in cells expressing human glutamate receptors. Neuropharmacology. 1997 Jan;36(1):1-11.

[7] Bond A, Monn JA, Lodge D. A novel orally active group 2 metabotropic glutamate receptor agonist: LY354740. Neuroreport. 1997 Apr 14;8(6):1463-6.

[8] Seeman P, Caruso C, Lasaga M (February 2008). „Dopamine partial agonist actions of the glutamate receptor agonists LY 354,740 and LY 379,268”. Synapse 62 (2): 154–8. DOI:10.1002/syn.20482. PMID 18000815.

[9] Fell MJ, Perry KW, Falcone JF, et al. (December 2009). „In vitro and in vivo evidence for a lack of interaction with dopamine D2 receptors by the metabotropic glutamate 2/3 receptor agonists 1S,2S,5R,6S-2-aminobicyclo[3.1.0hexane-2,6-bicaroxylate monohydrate (LY354740) and (-)-2-oxa-4-aminobicyclo[3.1.0] Hexane-4,6-dicarboxylic acid (LY379268)”]. J. Pharmacol. Exp. Ther. 331 (3): 1126–36. DOI:10.1124/jpet.109.160598. PMID 19755662.

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